Antitumor activity of 15-acetoxyscirpen-3,4-diol

Claridge, C.A.; Bradner, W.T.; Schmitz, H.

The Journal of Antibiotics 31(5): 485-486


DOI: 10.7164/antibiotics.31.485
Accession: 068515795

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The results of 3 experiments recording the effect of anguidine and 15-acetoxyscirpenol on P-388 leukemia in mice are given. 15-Acetoxyscirpenol showed activity at an 8-fold smaller dose than anguidine and produced a marked increase in median survival time (T/C > 200), indicative of greater antitumor effectiveness over a range of 3 doses, not evident with anguidine. The maximum tolerated dose for anguidine is 1.6 .apprx. 3.2 mg/kg per day and for 15-acetoxyscirpenol 0.8 mg/kg per day, suggesting at least a 2- to 4-fold difference in toxicity. This represents at least a 2-fold improvement in the therapeutic ratio. From the results of a cytotoxicity measurement employing HeLa human cervical cancer cells and L929 fibroblasts, it can be seen that the activity of 15-acetoxyscirpenol is about the same or perhaps slightly less than that of anguidine. The antitumor activity of a number of other analogs of anguidine prepared by microbiological or chemical transformations will be the subject of a further communication.